Synthesis, characterization and biological evaluation of acetazolamide, cycloserine and isoniazid condensed some novel phthalimide derivatives

Karthikeyan Elumalai , Mohammed Ashraf Ali , Manogaran Elumalai , Kalpana Eluri , Sivaneswari Srinivasan , Srinivasan Sivannan , Sujit Kumar Mohanthi
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引用次数: 12

Abstract

Background/aim

In the present study, a series of novel phthalimide derivatives synthesized because of its potent antimicrobial and antimycobacterial activity.

Method

Structurally modified phthalimide derivatives were prepared through condensation of substituted phthalic anhydride with corresponding acetazolamide, cycloserine and isoniazid with variable yields. Synthesized Compounds (6a–d), (7a–d) and (8a–d) analyzed for their structures, in vitro antimicrobial and antimycobacterial activity.

Result

Among the synthesized compounds, compound 6b, 7b and 8b was found to be the most potent against Gram-positive bacteria Bacillus subtilis, Gram-negative bacteria Escherichia coli, Mycobacterium tuberculosis CIP and M. tuberculosis H37Rv.

Conclusion

A series of novel phthalimide derivatives of biological interest were synthesized and analyzed, suggests that it an interesting compound compared to the current therapeutic agents and are considered to investigate further for the same.

乙酰唑胺、环丝氨酸和异烟肼缩合的新型邻苯二胺衍生物的合成、表征和生物学评价
背景/目的由于邻苯二甲酸亚胺具有较强的抗菌和抑菌活性,本研究合成了一系列新的邻苯二甲酸亚胺衍生物。方法通过取代邻苯二酸酐与相应的乙酰唑胺、环丝氨酸和异烟肼缩合制备结构修饰的邻苯二酸酐衍生物。对合成的化合物(6a-d)、(7a-d)和(8a-d)的结构、体外抗菌和抑菌活性进行了分析。结果化合物6b、7b和8b对革兰氏阳性菌枯草芽孢杆菌、革兰氏阴性菌大肠杆菌、结核分枝杆菌CIP和结核分枝杆菌H37Rv的抑制作用最强。结论合成并分析了一系列具有生物学意义的新型邻苯二胺衍生物,与现有的治疗药物相比,它是一种令人感兴趣的化合物,值得进一步研究。
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